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1. (WO1999052875) AMINE COMPOUNDS, THEIR PRODUCTION AND THEIR USE AS SOMATOSTATIN RECEPTOR ANTAGONISTS OR AGONISTS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/1999/052875 International Application No.: PCT/JP1999/001871
Publication Date: 21.10.1999 International Filing Date: 08.04.1999
Chapter 2 Demand Filed: 18.10.1999
IPC:
C07D 215/12 (2006.01) ,C07D 215/18 (2006.01) ,C07D 215/20 (2006.01) ,C07D 215/38 (2006.01) ,C07D 215/58 (2006.01) ,C07D 241/42 (2006.01) ,C07D 401/06 (2006.01) ,C07D 401/10 (2006.01) ,C07D 401/14 (2006.01) ,C07D 403/06 (2006.01) ,C07D 405/06 (2006.01) ,C07D 409/10 (2006.01) ,C07D 413/06 (2006.01) ,C07D 413/14 (2006.01) ,C07D 417/06 (2006.01) ,C07D 417/14 (2006.01) ,C07D 471/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
12
with substituted hydrocarbon radicals attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
18
Halogen atoms or nitro radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
20
Oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38
Nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
58
with hetero atoms directly attached to the ring nitrogen atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
241
Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
36
condensed with carbocyclic rings or ring systems
38
with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
40
Benzopyrazines
42
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
10
Spiro-condensed systems
Applicants:
SUZUKI, Nobuhiro [JP/JP]; JP (UsOnly)
KATO, Kaneyoshi [JP/JP]; JP (UsOnly)
TAKEKAWA, Shiro [JP/JP]; JP (UsOnly)
TERAUCHI, Jun [JP/JP]; JP (UsOnly)
ENDO, Satoshi [JP/JP]; JP (UsOnly)
TAKEDA CHEMICAL INDUSTRIES, LTD. [JP/JP]; 1-1, Doshomachi 4-chome Chuo-ku Osaka-shi Osaka 541-0045, JP (AllExceptUS)
Inventors:
SUZUKI, Nobuhiro; JP
KATO, Kaneyoshi; JP
TAKEKAWA, Shiro; JP
TERAUCHI, Jun; JP
ENDO, Satoshi; JP
Agent:
ASAHINA, Tadao ; Osaka Plant of Takeda Chemical Industries, Ltd. 17-85, Jusohonmachi 2-chome Yodogawa-ku Osaka-shi Osaka 532-0024, JP
LEWIN, John, Harvey; Elkington and Fife Prospect House 8 Pembroke Road Sevenoaks Kent TN13 1XR, GB
Priority Data:
10/34532804.12.1998JP
10/9642208.04.1998JP
Title (EN) AMINE COMPOUNDS, THEIR PRODUCTION AND THEIR USE AS SOMATOSTATIN RECEPTOR ANTAGONISTS OR AGONISTS
(FR) COMPOSES AMINES, LEUR PRODUCTION, ET LEUR UTILISATION COMME ANTAGONISTES OU AGONISTES DU RECEPTEUR DE LA SOMATOSTATINE
Abstract:
(EN) The present invention provides a compound of formula (I) wherein Ar represents an aromatic group which may be substituted; X represents methylene, S, SO, SO2 or CO; Y represents a spacer having a main chain of 2 to 5 atoms; n represents an integer of 1 to 5; i) R1 and R2 each represents a hydrogen atom or a lower alkyl which may be substituted, ii) R1 and R2 form, taken together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic ring which may be substituted, or iii) R1 or R2 together with -(CH2)n-N= form, bonded to a component atom of Ring B, a spiro-ring which may be substituted; Ring A represents an aromatic Ring which may be substituted; Ring B represents a 4- to 7-membered nitrogen-containing non-aromatic ring which may be further substituted by alkyl or acyl, with a proviso that X represents S, SO, SO2 or CO when Ring A has as a substituent a group represented by the formula: -NHCOR11 where R11 represents alkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or a group represented by the formula: -NHR12 where R12 represents alkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, or a salt thereof; which has an excellent somatostatin receptor binding inhibition action.
(FR) La présente invention concerne un composé de formule (I), dans laquelle: Ar représente un groupe aromatique éventuellement substitué; X représente méthylène, S, SO, SO2, ou CO; Y représente un espaceur avec une chaîne principale présentant 2 à 5 atomes; n représente un nombre entier entre 1 et 5; i) R1 et R2 représentent chacun un atome d'hydrogène ou un alkyle inférieur éventuellement substitué, ii) R1 et R2 forment avec l'atome d'azote adjacent un noyau hétérocyclique éventuellement substitué renfermant de l'azote, ou iii) R1 et R2 forment avec -(CH2)n-N=, lié à un atome du noyau B, un noyau spiro éventuellement substitué; le noyau A représente un noyau aromatique éventuellement substitué; le noyau B représente un noyau non aromatique renfermant de l'azote avec 4 à 7 chaînons, éventuellement substitué par alkyle ou acyle; à condition que X représente S, SO, SO2, ou CO, lorsque le noyau A présente, comme substituant, un groupe représenté par la formule: -NHCOR11, dans laquelle R11 représente alkyle, alkoxyalkyle, alkylthioalkyle, cycloalkyle, cycloalkylalkyle, aryle, arylalkyle, ou un groupe représenté par la formule: -NHR12, dans laquelle R12 représente alkyle, cycloalkyle, cycloalkylalkyle, aryle, ou arylalkyle, ou un sel de ceux-ci. Le composé de cette invention présente une excellente activité inhibitrice de la fixation du récepteur de la somatostatine.
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Designated States: AE, AL, AM, AU, AZ, BA, BB, BG, BR, BY, CA, CN, CU, CZ, EE, GD, GE, HR, HU, ID, IL, IN, IS, JP, KG, KR, KZ, LC, LK, LR, LT, LV, MD, MG, MK, MN, MX, NO, NZ, PL, RO, RU, SG, SI, SK, SL, TJ, TM, TR, TT, UA, US, UZ, VN, YU, ZA
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, SD, SL, SZ, UG, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)